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Art. -Nr.: HY-150769

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ZLM-66

ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC₅₀ of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC₅₀ value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3033486-43-7
Formel: C₂₄H₁₈F₃N₅O₃
Molecular Weight:481.43

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

ZLM-66 Chemical Structure

CAS. Nr.: 3033486-43-7

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

HIV-1 (WT)

13 nM (EC₅₀)

HIV-1 (K103N)

13 nM (EC₅₀)

HIV-1 (L100I)

24 nM (EC₅₀)

HIV-1 (E138K)

25 nM (EC₅₀)

HIV-1 (Y181C)

58 nM (EC₅₀)

HIV-1 (K103N+Y181C)

260 nM (EC₅₀)

HIV-1 (F227L+V106A)

27530 nM (EC₅₀)

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MT4	CC₅₀	26.45 μM Compound: B3; ZLM-66	Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay	[PMID: 35797898]

In Vitro

ZLM-66 (0.0016-125 μg/ml, 5 d) inhibits HIV-1 and HIV-1 mutant strains in MT-4 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

MT-4 cells infected with WT HIV-1 strain (IIIB) or HIV-2 (ROD)
Concentration:

125, 25, 5, 1, 0.2, 0.04, 0.008 and 0.0016 µg/ml
Incubation Time:

5 d
Result:

Exbited EC₅₀ value, CC₅₀ value and SI value of 13 nM, 26.45 μM and 2019.8 respectively against HIV-1 (IIIB). Inhibited L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, and K103N + Y181C (single and double HIV mutant strains) with EC₅₀s of 24, 13, 58, 760, 25, 27530 and 260 nM, respectively.

In Vivo

Zlm-66 (1-5 mg/kg; i.v. and p.o. once) shows good druggability and have a good effect in vivo after oral administration^[1].
1.19 Pharmacokinetic Parameters of ZLM-66 in rat^[1].
/tr> /tr>

	Rat IV 1 mg/kg	Rat PO 5 mg/kg
T_1/2 (h)	1.90±0.28	8.45±4.88
T_max (h)	0.08±0.00	6.67±1.15
C_max (ng/mL)	468.67±63.09	583.33±290.11
AUC_0-t (h*ng/ml)	891.94±79.30	4983.22±3220.11
AUC_0-∞ (h*ng/ml)	940.41±105.00	6594.05±1547.74
CL (ml/h/kg)	1072.31±120.40	791.14±210.66
MRT_0-t (h)	2.03±0.2	6.79±1.90
MRT_0-∞ (h)	2.48±0.35	13.92±6.44
F (%)		140.24

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Six- to 8-week-old male Sprague-Dawley rats (180−230 g)^[1]
Dosage:

1, 5 mg/kg
Administration:

Intravenous injection, oral gavage; 1-5 mg/kg; once
Result:

Possed a better in vivo effect of oral administration with half-life, plasma clearance and oral bioavailability of 8.45 h, 791.14 ml/h/kg and 140.24% respectively.

Chemical Information

CAS. Nr. 3033486-43-7
Molecular Weight 481.43
Formel C₂₄H₁₈F₃N₅O₃
SMILES

CN1C(CN(C=CC(C(F)(F)F)=C2OC3=CC(C#N)=CC(C4=CC(C)=CC=C4)=C3)C2=O)=NNC1=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhao LM, et al. Discovery of novel biphenyl-substituted pyridone derivatives as potent non-nucleoside reverse transcriptase inhibitors with promising oral bioavailability. Eur J Med Chem. 2022 Jun 30;240:114581. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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